New 5-HT_3 (Serotonin-3) Receptor Antagonists. II. Synthesis and Structure-Activity Relationships of Pyrimido[1,6-α]indoles
スポンサーリンク
概要
- 論文の詳細を見る
A series of pyrimido[1,6-α]indol-1(2H)-ones was prepared and evaluated for 5-HT_3 receptor antagonist activity. The compounds in this series were regarded as bioisosters of the pyrido[1,2-α]indol-6(7H)-ones previously reported. High potency was found for compounds having 5-methyl substituents on both the pyrimido[1,6-α]indole ring and the imidazole ring. Optimized members of this series, 8b and (+)-26a, were potent 5-HT_3 receptor antagonists as determined by measuring inhibition of the Bezold-Jarisch reflex in anesthetized rats (ED_<50> 0.6 and 0.8 μg/kg i.v., respectively), being equipotent to or more potent than FK 1052 (1) in the previous paper and 20- to 30-fold more potent than ondansetron (2).
- 社団法人日本薬学会の論文
- 1994-12-15
著者
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伊藤 清隆
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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高杉 寿
New Drug Research Laboratories Fujisawa Pharmaceutical Co., Ltd.,
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西野 重孝
New Drug Research Laboratories
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高杉 寿
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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加藤 眞行
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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山国 尚志
New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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Takasugi H
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd
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Takasugi H
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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西野 重孝
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Nishino S
Fujisawa Pharmaceutical Co. Ltd. Osaka Jpn
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山国 尚志
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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